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Kytril

中文名称
——
中文别名
——
英文名称
Kytril
英文别名
1-methyl-N-[(1R,5S)-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl]indazole-3-carboxamide;hydrochloride
Kytril化学式
CAS
——
化学式
C18H25ClN4O
mdl
——
分子量
348.9
InChiKey
QYZRTBKYBJRGJB-PCMHIUKPSA-N
BEILSTEIN
——
EINECS
——
  • 物化性质
  • 计算性质
  • ADMET
  • 安全信息
  • SDS
  • 制备方法与用途
  • 上下游信息
  • 反应信息
  • 文献信息
  • 表征谱图
  • 同类化合物
  • 相关功能分类
  • 相关结构分类

计算性质

  • 辛醇/水分配系数(LogP):
    2.74
  • 重原子数:
    24
  • 可旋转键数:
    2
  • 环数:
    4.0
  • sp3杂化的碳原子比例:
    0.56
  • 拓扑面积:
    50.2
  • 氢给体数:
    2
  • 氢受体数:
    3

ADMET

毒理性
  • 在妊娠和哺乳期间的影响
◉ 母乳喂养期间使用总结:目前没有关于在哺乳期间使用格雷司琼的信息。在获得更多信息之前,哺乳期间应谨慎使用格雷司琼。可能更倾向于使用另一种药物。 ◉ 对哺乳婴儿的影响:截至修订日期,没有找到相关的已发布信息。 ◉ 对泌乳和母乳的影响:一位正在给一个8个月大婴儿哺乳的母亲,每天6到8次,因阑尾炎入院接受手术。在手术过程中,她接受了格雷司琼、头孢唑林、酮咯酸、罗库溴铵、琥珀胆碱和舒芬太尼。患者还接受了两次静脉注射丙泊酚150毫克,随后不久又注射了50毫克。术后,她接受了对乙酰氨基酚、头孢唑林、布洛芬和泮托拉唑,以及按需使用的氧可酮和晕海宁。手术22小时后,母亲第一次挤出乳汁,发现乳汁呈浅绿色。使用未经验证的分析方法对绿色乳汁进行分析,未检测到丙泊酚。绿色在术后第4天消失,当她恢复哺乳时。作者判断,绿色可能是由于丙泊酚或其代谢物引起的。
◉ Summary of Use during Lactation:No information is available on the use of granisetron during breastfeeding. Until more data become available, granisetron should be used with caution during breastfeeding. An alternate drug may be preferred. ◉ Effects in Breastfed Infants:Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk:A woman nursing an 8-month-old infant 6 to 8 times daily was admitted to the hospital for an appendectomy. During the procedure she received granisetron, cefazolin, ketorolac, rocuronium, succinylcholine, and sufentanil. The patient also received 2 boluses of intravenous propofol of 150 mg followed shortly thereafter by a 50 mg dose. Postoperatively, she was receiving acetaminophen, cefazolin, ibuprofen, and pantoprazole, as well as oxycodone and dimenhydrinate as needed. Twenty-two hours after the procedure, the mother extracted milk for the first time and noted it to be light green in color. Analysis of the green milk using a nonvalidated assay detected no propofol. The green color faded and was absent by postoperative day 4 when she resumed breastfeeding. The authors judged that the green color was possibly caused by propofol or one of its metabolites.
来源:Drugs and Lactation Database (LactMed)

文献信息

  • HETEROAROMATIC COMPOUNDS FOR USE AS HIF INHIBITORS
    申请人:Härter Michael
    公开号:US20110301122A1
    公开(公告)日:2011-12-08
    The present application relates to novel substituted aryl compounds, processes for their preparation, their use for treatment and/or prevention of diseases and their use for the preparation of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be carried out as monotherapy or also in combination with other medicaments or further therapeutic measures.
    本申请涉及新型取代芳基化合物,其制备方法,它们用于治疗和/或预防疾病以及用于制备治疗和/或预防疾病的药物,特别是用于治疗和/或预防过度增殖和血管生成性疾病以及那些由于代谢适应缺氧状态而引起的疾病。这种治疗可以作为单独治疗进行,也可以与其他药物或进一步的治疗措施结合使用。
  • Aryl compounds with aminoalkyl substituents and their use
    申请人:Härter Michael
    公开号:US20110312930A1
    公开(公告)日:2011-12-22
    The present application relates to novel aryl compounds with aminoalkyl substituents, to processes for their preparation, to their use for treatment and/or prevention of diseases and to their use for the preparation of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be carried out as monotherapy or also in combination with other medicaments or further therapeutic measures.
    本申请涉及具有氨基烷基取代基的新型芳基化合物,涉及其制备方法,涉及它们用于治疗和/或预防疾病以及用于制备治疗和/或预防疾病的药物的用途,特别是用于治疗和/或预防过度增殖和血管生成性疾病以及那些由于代谢适应低氧状态而引起的疾病。这种治疗可以作为单独治疗进行,也可以与其他药物或进一步的治疗措施结合使用。
  • NEW ANTIBODY DRUG CONJUGATES (ADCS) AND THE USE THEREOF
    申请人:SEATTLE GENETICS, INC.
    公开号:US20150023989A1
    公开(公告)日:2015-01-22
    The present application relates to new antibody drug conjugates (ADCs) of N,N dialkylauristatins directed against the target FGFR2, drug metabolites of said ADCs, a method for producing said ADCs, the use of said ADCs for the treatment and/or prevention of illnesses as well as the use of said ADCs for producing pharmaceuticals for the treatment and/or prevention of illnesses, particularly of hyperproliferative and/or angiogenic diseases such as carcinosis. Such treatments can be carried out as monotherapy or in combination with other pharmaceuticals or additional therapeutic measures.
    本申请涉及针对FGFR2靶点的新抗体药物结合物(ADCs),所述ADCs的药物代谢产物,生产所述ADCs的方法,利用所述ADCs治疗和/或预防疾病以及利用所述ADCs生产用于治疗和/或预防疾病的药物,特别是治疗高增殖和/或血管生成性疾病如癌症。这种治疗可以作为单药疗法进行,也可以与其他药物或额外的治疗措施结合使用。
  • Substituted heterocyclylbenzylpyrazoles and use thereof
    申请人:HÄRTER Michael
    公开号:US20120028950A1
    公开(公告)日:2012-02-02
    The present application relates to novel substituted 1-[3-(heterocyclyl)benzyl]-1H-pyrazole derivatives, to processes for preparation thereof, to use thereof for treatment and/or prevention of diseases and to use thereof for production of medicaments for treatment and/or prevention of diseases, more particularly for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be effected in the form of monotherapy or else in combination with other medicaments or further therapeutic measures.
    本申请涉及新颖的取代的1-[3-(杂环基)苄基]-1H-吡唑衍生物,其制备方法,用于治疗和/或预防疾病以及用于生产治疗和/或预防疾病的药物的用途,更具体地用于治疗和/或预防过度增殖和血管生成性疾病以及那些由于代谢适应缺氧状态而引起的疾病。这种治疗可以以单药疗法形式进行,也可以与其他药物或进一步的治疗措施结合使用。
  • [EN] 1-AMIDO-4-PHENYL-4-BENZYLOXYMETHYL-PIPERIDINE DERIVATIVES AND RELATED COMPOUNDS AS NEUROKININ-1(NK-1) ANTAGONISTS FOR THE TREATMENT OF EMESIS, DEPRESSION, ANXIETY AND COUGH<br/>[FR] DERIVES DE 1-AMIDO-4-PHENYL-4-BENZYLOXYMETHYL-PIPERIDINE ET COMPOSES ASSOCIES EN TANT QU'ANTAGONISTES DE LA NEUROKININE-1(NK-1) DANS LE TRAITEMENT DES VOMISSEMENTS, DE LA DEPRESSION, DE L'ANGOISSE ET DE LA TOUX
    申请人:SCHERING CORP
    公开号:WO2004004722A1
    公开(公告)日:2004-01-15
    Disclosed are NK1 antagonists having the formula: Also disclosed are uses of compounds of formula (I) for the manufacture of a medicament for treating a number of physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
    揭示了具有以下结构式的NK1拮抗剂:还揭示了利用结构式(I)化合物制备用于治疗多种生理紊乱、症状或疾病的药物,包括恶心、抑郁、焦虑和咳嗽。
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